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Modafinil – selective alpha-1-adrenomimetic mainly central action. There is evidence that modafinil acts through the glutamatergic system and increases the level of synthesis of glutamic acid, inhibiting the release of GABA. The drug was developed for the treatment of narcolepsy. In 1998, modafinil was the first drug in its class to help wakefulness and resolved in the US. During the trials, patients who took modafinil stayed awake for 28 hours, keeping attention and working capacity. According to the media, the drug is actively used in the armies of the United States and Britain to correct the performance, primarily for pilots. Modafinil, almost without affecting physical performance, reduces the need for sleep. The only indication for his appointment in clinical medicine was narcolepsy. Can be effectively used to increase concentration.
This substance can stimulate brain activity, removing drowsiness. Of course, this property is manifested not only in patients with narcolepsy, but also in any person whose activity and attention are reduced as a result of lack of sleep. This leads to the danger of abuse of modafinil. However, researchers are trying to prove that the drug is not addictive and has no drug potential. The remedy works like amphetamines, increasing the release of dopamine and norepinephrine. But, also, in the hypothalamus, the level of histamine rises. In general, the exact mechanism of action of modafinil on the body has not yet been described.
Application in medicine
Modafinil is a psychostimulant. It was developed in the late 80s of the last century by the American manufacturer of medicines Cephalon for the treatment of narcolepsy – a disease in which people suddenly fall asleep during the day. Approximately 0.02-0.03% of the population suffers from narcolepsy. Modafinil is used in about 20 countries.
In Finland, there is no marketing license for modafinil, but Fimea has issued a special permit for the treatment of narcolepsy with modafinil in Finland. The standard dose of modafinil for the treatment of narcolepsy is 200 milligrams in the morning.
Modafinil is also used to treat other conditions other than narcolepsy, which also cause daytime drowsiness. In addition, sometimes it is used to treat disorders with memory and attention deficit, Alzheimer’s disease and depression.
Studies of modafinil drugs in patients with various other pathological conditions are under way. For example, an experimental treatment is performed:
- attention deficit hyperactivity disorder in children;
- disorders of mental activity in patients with multiple sclerosis and those who underwent chemotherapy;
- drowsiness and fatigue in patients with certain liver diseases;
- and so on.
However, these are only hypotheses, many of which are not confirmed. In many cases, the side effects of such therapy are more significant than a positive effect on health.
Issue modafinil in tablets of different dosage. For example, each tablet of means Alertec or Modalert contains 100 mg of this active substance. The instruction of this drug informs that it should be taken twice a day – in the morning and in the afternoon (around noon). At the reception is offered from 1 to 2 tablets. The exact scheme of treatment prescribes the doctor. The effect of the next dose becomes noticeable, approximately, in an hour, after its reception.
- Diseases of the heart;
- Cirrhosis of the liver;
- Allergies to any pill components with modafinil;
- Pregnancy and lactation;
Patients should be aware that such treatment can not be combined with taking alcohol, yohimbine drugs (stimulants of sexual activity). Modafinil reduces the effectiveness of some contraceptives.
By classification, modafinil refers to doping drugs. Its effect on sports results has not been studied, however, based on the effects of this drug, it is assumed that it improves endurance and quickness. It is known that in bodybuilding it is used to reduce the fat content due to the effect of suppressing appetite.
Properties and mechanism of action
The mechanism of action of modafinil differs from the mechanism of action of amphetamine and ephedrine or other similar psychostimulants. Modafinil also does not form in the human body from derivatives of amphetamine or ephedrine. Adafinil, an older drug than modafinil, is a drug similar to modafinil in structure and effects.
Modafinil affects different parts of the brain. Probably the most important effect is an increase in the speed of mental reactions. This effect refers to the lower part of the intermediate brain, the hypothalamus, where the activation of the neural pathways in which orexin / hypocretin action plays an important role in the regulation of sleep-wakefulness as mediators occurs.
In addition, it activates the sympathetic alpha-1 receptors of the central nervous system, increases the activity of stimulation of glutamine and histamine transmitters, and also enhances the effects of serotonin in the cerebral cortex.
In addition, it reduces the activity of those inhibitory nerve cells in which gamma-aminobutyric acid acts as a transmitter. Modafinil does not lead to excitation of the dopamine system in the central nervous system, which is the most important effect of amphetamines.
When testing a new drug, scientists noted the absence of side effects characteristic of traditional stimulants of the time – amphetamines, ritalin and ephedrine. Due to a special mechanism of action, modafinil does not cause a “recoil effect” like amphetamine, and does not enter into a nervous state like ritalin, while retaining the main effect – increasing the time of wakefulness, relieving stress, fatigue and increasing cognitive abilities. Modafinil is positioned as a remedy for drowsiness, and in this area practically has no equivalent competitors – users often describe the effect of the drug as “I never sleep, I never eat.” The effects of increasing productivity and cognitive improvement have led to a lot of research, and the Swedish neuroscientist and transhumanist Anders Sandberg, in his speech at the TransVision conference, described modafinil as “perhaps the most approached to date to create an intelligence enhancer drug.” Of the negative effects can be noted frequent headache, dry mouth and the inherent effects of many nootropic drugs excessive irritability, the so-called “effect of the internal snob”.
Most often, patients complain of:
- Dry mouth;
- Nausea or diarrhea;
- Nasal congestion;
- Back pain;
Modafinil can lead to the effect of pleasure and addiction, but to a much lesser extent than amphetamines. It is well tolerated in therapeutic doses, but side effects may include insomnia, headaches, nervousness, agitation, aggressiveness, increased blood pressure and symptoms from the heart.
Insomnia can become an obvious consequence of taking modafinil. Such reactions often disappear themselves within a few days from the start of treatment or with a decrease in dosage.
In addition, the following are possible:
- Allergic reactions of varying severity;
- Violations of the functions of the liver;
- Ulceration of the oral mucosa;
- Increased body temperature;
If these symptoms appear, stop using modafinil and consult a doctor who prescribes it. In some cases, hospitalization is required.
When an overdose occurs, a strong nervous excitement, palpitations, a rise in blood pressure. A person needs specialist examination and medical assistance.
Since this substance is an active component – it is based on the production of such drugs as:
Of course, such medicines always cause increased interest. Many people see in the description of the drug what they like: “a stimulant that removes drowsiness and improves intellectual functions” – and all other “details” are skipped or recognized (completely groundless) insignificant.
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